PI-3065

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Technical Data

Molecular Weight 506.64 Storage powder
Formula

C27H31FN6OS

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CAS No. 955977-50-1 Synonyms N/A
Solubility (25°C) * In vitro DMSO 50 mg/mL warmed (98.68 mM)
Water Insoluble
Ethanol Insoluble
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 6-((4-(cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)-4-morpholinothieno[3,2-d]pyrimidine

Biological Activity

Description PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
Targets
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
15 nM 1078 nM
In vitro PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ. [1]
In vivo In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, PI-3065 prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies. [1]
Features  

Protocol (Only for Reference)

Cell Assay:

[1]

Cell lines 4T1 cells
Concentrations ~10 μM
Incubation Time 48 hours
Method

Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ inhibitors, then washing and MTS staining are carried out after 48 h culture.

Animal Study:

[1]

Animal Models Female WT BALB/c mice bearing 4T1 tumors
Formulation 0.5% methylcellulose with 0.2% Tween 80
Dosages 75 mg/kg, once daily
Administration p.o.
 

References

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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